EA200870384A1 - 3,7-DIAMINO-10H-PHENOTIAZINE SALTS AND THEIR APPLICATION - Google Patents

3,7-DIAMINO-10H-PHENOTIAZINE SALTS AND THEIR APPLICATION

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Publication number
EA200870384A1
EA200870384A1 EA200870384A EA200870384A EA200870384A1 EA 200870384 A1 EA200870384 A1 EA 200870384A1 EA 200870384 A EA200870384 A EA 200870384A EA 200870384 A EA200870384 A EA 200870384A EA 200870384 A1 EA200870384 A1 EA 200870384A1
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EA
Eurasian Patent Office
Prior art keywords
6alkyl
compounds
halogenated
independently selected
diamino
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EA200870384A
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Russian (ru)
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EA014552B1 (en
Inventor
Клод Мишель Вишик
Дженет Элизабет Рикард
Чарльз Роберт Харрингтон
Дэвид Хорсли
Джон Мервин Дэвид Стори
Колин Маршалл
Джеймс Питер Синклер
Томас Кравен Баддели
Original Assignee
Уиста Лэборэтэриз Лтд.
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Application filed by Уиста Лэборэтэриз Лтд. filed Critical Уиста Лэборэтэриз Лтд.
Publication of EA200870384A1 publication Critical patent/EA200870384A1/en
Publication of EA014552B1 publication Critical patent/EA014552B1/en

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    • C—CHEMISTRY; METALLURGY
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    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/18—[b, e]-condensed with two six-membered rings
    • C07D279/20—[b, e]-condensed with two six-membered rings with hydrogen atoms directly attached to the ring nitrogen atom
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/18—[b, e]-condensed with two six-membered rings
    • C07D279/22—[b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom
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    • C09B21/00—Thiazine dyes
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    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
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  • Health & Medical Sciences (AREA)
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Abstract

Это изобретение относится в общем к области соединений фенотиазина, и более подробно, к определенным стабильным восстановленным соединениям фенотиазина, а именно, определенным соединениям 3,7-диамино-10Н-фенотиазна (DAPTZ) следующей формулы:каждый из Rи Rнезависимо выбран из -Н, Салкил, Салкенил и галогенированый Салкил; каждый их Rи Rнезависимо выбран из -Н, Салкил, Салкенил и галогенированый Салкил; каждый их Rи Rнезависимо выбран из -Н, Салкил, Салкенил и галогенированый Салкил; каждый из НХи НХнезависимо являются протонной кислотой; и его фармацевтически приемлемые соли, сольваты и гидраты. Эти соединения применимы в качестве лекарственных средств, например, для лечения тауопатий, таких как болезнь Альцгеймера, и так же в качестве пролекарств для соответствующих окисленных тиониниевых лекарственных средств (например, метилтионин хлорида, МТС).This invention relates in general to the field of phenothiazine compounds, and in more detail, to certain stable reduced phenothiazine compounds, namely, certain 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of the following formula: each of R 3 and R 5 is independently selected from —H, C1-6 alkyl, C2-6alkenyl and halogenated C1-6 alkyl; each of them is independently selected from —H, C1-6alkyl, Salkenyl, and halogenated C1-6alkyl; each of them is independently selected from —H, C1-6alkyl, Salkenyl, and halogenated C1-6alkyl; each of NHI, NH is independently a proton acid; and its pharmaceutically acceptable salts, solvates and hydrates. These compounds are useful as medicaments, for example, for the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methylthionine chloride, MTS).

EA200870384A 2006-03-29 2007-03-28 3,7-diamino-10h-phenothiazine salts and their use EA014552B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US78669006P 2006-03-29 2006-03-29
PCT/GB2007/001103 WO2007110627A2 (en) 2006-03-29 2007-03-28 3,7-diamino-10h-phenothiazine salts and their use

Publications (2)

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EA200870384A1 true EA200870384A1 (en) 2009-04-28
EA014552B1 EA014552B1 (en) 2010-12-30

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US (3) US7888350B2 (en)
EP (1) EP2013191B3 (en)
JP (3) JP5520043B2 (en)
KR (1) KR100983301B1 (en)
CN (5) CN101460472B (en)
AT (1) ATE478058T3 (en)
AU (1) AU2007231124B2 (en)
CA (1) CA2646163C (en)
DE (1) DE602007008550D1 (en)
DK (1) DK2013191T6 (en)
EA (1) EA014552B1 (en)
ES (1) ES2349322T7 (en)
HK (4) HK1126480A1 (en)
HR (1) HRP20100614T4 (en)
IL (2) IL194516A (en)
MY (1) MY143757A (en)
PL (1) PL2013191T6 (en)
PT (1) PT2013191E (en)
WO (1) WO2007110627A2 (en)

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